949485-81-8Relevant articles and documents
2-Halobenzoyl chlorides in the synthesis of [1,3,4]thiadiazolo[3,2-a]quinazolin-5-one derivatives
Shlenev,Tarasov,Filimonov,Agat’ev,Danilova,Suponitskii, K. Yu.
, p. 1870 - 1877 (2018/02/06)
New nitro and sulfonamide derivatives of [1,3,4]thiadiazolo[3,2-a]quinazolin-5-one have been synthesized by cyclocondensation of 1,3,4-thiadiazol-2-amines with 2-halobenzoyl chlorides containing electron-withdrawing substituents in positions 3, 4, and 5. An improved procedure has been proposed for the preparation of intermediate 2-fluoro-N-(5-methyl-1,3,4-thiadiazol-2-yl)benzamides containing a sulfamoyl group in the 5-position via selective acylation of 5-methyl-1,3,4-thiadiazol-2-amine with 5-chlorosulfonyl-2-fluorobenzoyl chloride, followed by sulfonylation of amines.
Synthesis of new sulfonamide derivatives of thiazolo[3,2-a]quinazolin-5-one
Shlenev,Filimonov,Tarasov,Danilova,Agat’ev
, p. 69 - 75 (2017/01/11)
A general procedure has been proposed for the synthesis of thiazolo[3,2-a]quinazolin-5-one derivatives containing a sulfonamide group on C7via intramolecular nucleophilic substitution of halogen in 2-halo-5-sulfamoyl-N-(1,3-thiazol-2-yl)benzami
SULFAMOYL-ARYLAMIDES AND THE USE THEREOF AS MEDICAMENTS FOR THE TREATMENT OF HEPATITIS B
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Page/Page column 63-64, (2014/03/25)
Inhibitors of HBV replication of Formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein B, R1, R2 and R4 have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy.